Prospects and challenges of the development of lipoprotein-based formulations for anti-cancer drugs

This review evaluates drug delivery systems that involve intact plasma lipoproteins or some of their components. These complex macromolecules transport highly water-insoluble compounds (cholesteryl esters and triacylglycerols) in their natural environment - a property that renders them ideal carriers of hydrophobic drugs. Particular emphasis is placed on the application of lipoproteins as drug delivery agents in cancer chemotherapy. The history and present activity regarding lipoprotein-based formulations are reviewed, with the primary focus on the smaller sized (low and high density) lipoprotein-based formulations and their potential clinical and commercial value. The use of both native and synthetic lipoproteins as drug delivery agents are discussed from the standpoint of therapeutic efficacy, as well as commercial feasibility. The advantages of lipoprotein-based drug delivery formulations are compared with other drug delivery models, with the primary focus on liposomal preparations. Finally, an expert opinion is provided, regarding the potential use of lipoprotein-based formulations in cancer treatment, taking into consideration the major advantages (biocompatibility, safety, drug solubility) and the barriers (manufacturing protein components, financial interest, investments) to their commercial development.